Objective To study the effect of fat emulsion intravenous infusion on serum free fatty acids(FFAs) in rats.Methods 24 male Wistar rats were divided randomly into 3 groups,8 rats in each group.(1)Control group(NS),the rats were infused with normal saline intravenously and regular chow;(2)Group LCT,infused with 10% intralipid fat emulsion intravenously;(3)Group MCT/LCT,infused with 10% lipofundin fat emulsion. Group LCT and group MCT/LCT were continuously received equal calorie,nitrogen and volemin in 'All-in-One'solutions. Serum samples were drawn on the 8th day after PN for fatty acid determination. Results The FFAs in Group LCT and group MCT/LCT were remarkably higher than that in control group, but no difference between Group LCT and group MCT/LCT. Conclusions Fat emulsion intravenous infusion can increase the serum free fatty acids considerately.

OBJECTIVE:To study the bioequiavailability of domestic roxithromycin tablets and imported ones.METH?ODS:20male healthy volunteers took single dose of150mg roxithromycin tablet orally in a random crossover design,blood concentrations were determined by LC-MS.RESULTS:The main pharmacokinetic parameters of domestic and imported tablets were determined respectively as follows,AUC 0～72 were(72.81?23.85)(mg?n)/L and(72.63?20.86)(mg?h)/L,AUC 0～∞ were(74.41?24.45)(mg?h)/L and(74.42?24.45)(mg?h)/L,C max were(6.46?1.51)mg/L and(6.58?1.55)mg/L,t max were(1.9?0.5)h and(1.8?0.5)h,t 1/2 were(13.56?1.35)h and(14.18?1.50)h,the relative bioavailability of the homemade tablet to imported one was(99.8?11.2)%.CONCLUSIONS:Domestic and imported roxithromycin are bioequivalent.

Tetrazanbigen (TNBG) is a novel synthetic antitumor drug with significant antitumor effects on common solid tumors in vitro and in vivo. It may lead to death of cancer cells through a tumor-associated lipoidosis mechanism, and result in lipid droplets (LDs) accumulation at the cytoplasm. In this study, the effects of TNBG on protein expression in human hepatocellular carcinoma cell line QGY-7701 were studied for elucidating its antitumor mechanism. The proteins extracted from TNBG-treated human hepatocellular carcinoma cell line QGY-7701 were analyzed and compared with control cells by two-dimensional gel electrophoresis. The differential proteins were identified by matrix-associated laser desorption ionization time-of-flight mass (MALDI-TOF-MS) spectrometry. Two proteins of interest, the levels of which were significantly increased in TNBG-treated cells, were further characterized by Western blot analysis. The results showed a total of 846+/-23 spots in control cells and 853+/-30 spots in TNBG-treated cells. Twenty-six up-regulated or down-regulated proteins were found by analyzing differential proteomic 2-DE map. Eleven of them were identified by mass spectrometry. They were protein disulfide-isomerase precursor, 94 kD glucose-regulated protein, heat shock protein (HSP) 90-alpha, ATP-citrate lyase, HMG-CoA reductase, glucose-6-phosphate 1-dehydrogenase, very-long-chain specific acyl-CoA dehydrogenase, squalene synthetase, sterol regulatory element-binding protein 1, fructose-bisphosphate aldolase A, and peroxiredoxin-1. These up-regulated or down-regulated proteins are mostly related to lipid metabolism. The TNBG antitumor mechanism is probably to influence tumor lipid metabolism, resulting in accumulation of LDs in tumor cells.
Antineoplastic Agents/*pharmacology ; Azo Compounds/*pharmacology ; Carcinoma, Hepatocellular/*pathology ; Cell Line, Tumor ; Gonanes/*pharmacology ; Liver Neoplasms/*pathology ; Proteins/*metabolism ; Proteome

OBJECTIVETo investigate the effects and mechanisms of cordycepin,an effective component of cordyceps militaris, on renal interstitial fibrosis (RIF) and its related eIF2α/TGF-β/Smad signaling pathway.

METHODFirstly, 15 C57BL/6 mice were randomly divided into 3 groups,the control group (Group A), the model group (Group B) and the cordycepin-treated group (Group C). After renal interstitial fibrotic model was successfully established by unilateral ureteral obstruction (UUO), the mice in Group C were intraperitoneally administrated with cordycepin(5 mg x kg(-1) d(-1)) and the ones in Group A and B were administrated with physiological saline for 5 days. At the end of the study, the obstructed kidneys were collected and detected for the pathological changes of RIF, and the mRNA expressions of collagen type I (Col I) and α-smooth muscle actin (α-SMA) in the kidney by Northern blot. Secondly, after renal tubular epithelial (NRK-52E) cells cultured in vitro were exposed to transforming growth factor (TGF) -β with or without cordycepin, the mRNA expressions of Col I and collagen type IV( Col IV) by Northern blot, and the protein expressions of eukaryotic initiation factor 2α (eIF2α), phosphorylated eIF2α ( p-eIF2α), Smad2/3 and phosphorylated Smad2/3 (p-Smad2/3) were tested by Western blot.

RESULTIn vivo, cordycepin alleviated RIF in model mice, including improving fibrotic pathological characteristics and mRNA expressions of Col I and α-SMA. In vitro, cordycepin induced the high expression of p-elF2α, and inhibited the expressions of p-Smad2/3, Col I and Col IV induced by TGF-β in NRK-52E cells.

CONCLUSIONCordycepin attenuates RIF in vivo and in vitro, probably by inducing the phosphorylation of eIF2α, suppressing the expression of p-Smad2/3, a key signaling molecule in TGF-β/Smad signaling pathway, and reducing the expressions of collagens and α-SMA in the kidney.

Actins ; analysis ; Animals ; Deoxyadenosines ; pharmacology ; Fibrosis ; Kidney ; drug effects ; pathology ; Male ; Mice ; Mice, Inbred C57BL ; Phosphorylation ; Protein-Serine-Threonine Kinases ; physiology ; Signal Transduction ; drug effects ; Smad Proteins ; physiology ; Transforming Growth Factor beta ; antagonists & inhibitors ; physiology

0.05).The protein and mRNA expression of MIP-2 in high glucose group significantly increased after culture for 4 h,and guadually decreased then.The protein and mRNA expression of MCP-1 began to increase significantly after culture for 8 h,reached peak at 12 h,and slightly decreased after culture for 24 and 48 h. Conclusion High glucose promotes the protein and mRNA expression of MIP-2 and MCP-1 from mouse peritoneal macrophages cultured in vitro,which indicates that high glucose may delay the wound healing by increasing the expression of chemokines in diabetic mice.

Objective To study the effects of nuclear factor-?B(NF-?B)decoy oligodeoxynucleotide(ODN)on the preeclamptic umbilical serum induced expression of precollagen Ⅰ,Ⅲ mRNA and tumor necrosis factor-?(TNF-?)in cultured human umbilical artery smooth muscle cells (HUASMC).Methods Primary cultured HUASMC of normal pregnancy were divided into four groups: group A(HUASMC were incubated with umbilical serum of normal pregnancy);group B(HUASMC were incubated with umbilical serum of preeclampsia);group C(HUASMC were transfected with NF-?B cis decoy ODN 48 h before incubation with umbilical serum of preeclampsia);group D(HUASMC were transfected with NF-?B scramble ODN 24 h before incubation with umbilical serum of preeclampsia).NF-?B cis decoy ODN and NF-?B scramble ODN were transfected with cationic lipofectamine to the latter two groups,respectively.The proliferation of human umbilical artery smooth muscle cells was evaluated by methyl thiazolyl tetrazolium and the apoptosis was analyzed by flow cytometry.The expression levels of precollagen Ⅰ,Ⅲ mRNA were detected by RT-PCR,the expression levels of TNF-? were detected by western blot.Results(1)The proliferation of group B(0.19?0.02)and group D(0.18?0.03)was significantly increased as compared with those of group A(0.11?0.02)and group C(0.14?20.02)(P0.05).(5)The expression of TNF-? of group B(0.74?0.11),group C(0.36?0.09)and group D(0.79?0.12)were significantly higher than that of group A(0.15?0.03)(P0.05).Conclusions NF-?B cis decoy ODN could down-regulate the proliferation,as well as the expression levels of precollagen and TNF-? of HUASMC induced by umbilical serum of preeclampsia.NF-?B may play an important role in the pathogenesis of placental artery abnormalities in preeclampsia.

OBJECTIVETo study the curative effect of postural reduction with instrumental reduction in treatment of flexion-distraction thoracolumbar fractures.

METHODSA retrospective study was performed on 43 patients with single thoracolumbar flexion-distraction fractures admitted from August 2009 to August 2011, included 28 males and 15 females with an average age of 44 years old (34 to 56 years old). All patients were treated with postural reduction with instrumental reduction. The kyphosis (Cobb angle) recovery of injured vertebral height and complication were analyzed. The visual analogue scale(VAS) and com-plications were followed up and recorded.

RESULTSThere was no difference in recovery of injured vertebral posterior height among preoperative, 1 week and 1 year after operation (P > 0.05). There were significantly difference in kyphosis (Cobb angle) and recovery of injured vertebral anterior height between preoperative and postoperative at 1 week (P < 0.05). There was no difference in kyphosis (Cobb angle) and recovery of injured vertebral anterior height between 1 week and 1 year after operation (P > 0.05). VAS significantly improved from preoperative (7.2 +/- 1.2) to (0.8 +/- 0.7) at 1 year after operation (t = 18.47, P < 0.001).

CONCLUSIONPostural reduction with instrumental reduction is effective for thoracolumbar flexion-distraction fractures and it is beneficial to the recovery of vertebral height and saggital alignment.

Adult ; Female ; Fracture Fixation, Internal ; adverse effects ; Humans ; Male ; Middle Aged ; Retrospective Studies ; Spinal Fractures ; physiopathology ; surgery ; Thoracic Vertebrae ; injuries ; physiopathology ; surgery ; Visual Analog Scale

AIM To establish the HPLC fingerprints of Yupingfeng Powder aqueous decoction and to determine the contents of nine constituents.METHODS The analysis of aqueous decoction was developed on a 30 ℃ thermostatic Hypersil ODS column (250 mm × 4.6 mm,5 μm),with the mobile phase comprising of acetonitrile-water flowing at 1.0 mL/min in a gradient elution manner,and the detection wavelength was set at 220 nm.RESULTS There were fifteen common peaks in the fingerprints of ten batches of samples,with the similarities of more than 0.95.Nine of them were identified as prim-O-glucosylcimifugin,calycosin-7-O-β-D-glucoside,cimifugin,4'-O-β-glucopyranosyl-5-O-methylvisamminol,psoralen,calycosin,sec-O-glucosylhamaudol,formononetin and atractylon,which showed good linear relationships within their own ranges (r ≥ 0.999 7),the average recoveries were 97.91％-99.81％ with the RSDs of 0.58％-1.27％.CONCLUSION This stable and reliable method can beused for the quality control of Yupingfeng Powder aqueous decoction.

AIM: To compare the pharmacokinetics and relative bioavailability of the domestic and imported sustained-release tablets of gliclazide in healthy volunteers. METHODS:The study was performed by an four-period crossover design with singledose and multiple-dose administration. The plasmadrug concentrations of twenty male healthy volunteers were determined by liquid chromatography with mass spectrum detector method (LC-MS). RESULTS:The pharmacokinetic parameters after a single oral dose of the domestic and imported gliclazide tablets were (7.2+s 1.5) h and (6.9 +1.4) h for tmax, (13.4 ±1.2) h and (13.7 +1.3) h for t1/2, (2.4 +0.8) mg ·L-1and (2.3 ±0.6) mg· L-1 forcmax, (48 ±14)mg · h · L-1 and (48 +14) mg· h · L-1 forAUC0-60,(51+15) mg· h· L-1 and (50±14) mg· h· L-1for AUC0-∞, (22.4 ± 1.9 ) h and (22.8 ± 1.9 ) h for MRT, respectively. The steady state pharmacokinetic parameters after multiple doses of the domestic and imported gliclazide tablets were (6. 1 ± 1.4) h and (6.5+1.4) h for tmax, (4.6±0.9) mg· L-1 and (4.7±1.1) mg· L-1 for cmax, (0.23 ±0.08) mg ·L-1and (0.26±0.08) mg· L-1 forcmin, (1.6±0.3) mg·L-1 and (1.6±0.3) mg · L-1 for mean value of steady plasma-drug concentration (cav),(94±19) mg· h · L-1 and (95 ±20) mg · h · L-1forAUCss, (282 ±33)% and (283 ±43)% for degree of fluctuation DF ), respectively. The relative bioavailability of the domestic gliclazide tablet to the imported gliclazide tablet following a single and multiple dose were ( 102 ± 9) % and (99 ± 10 ) %, respectively. Main pharmacokinetic parameters between the two formulations in both single and multiples dose studies showed no statistical difference ( P >0.05 ). CONCLUSION: The result of two one side t-test shows that the two formulations are bioequivalent.

Objective To explore the roles of serum TLR-4, TNF-αand IL-6 in neonates with preterm birth. Methods A total of 120 neonates from neonatology department in the Xingtai People's Hospital were selected and divided into full-term group (n=40), premature rupture of fetal membranes (n=40) and idiopathic preterm group (n=40) based on the gestational age. The peripheral venous blood was collected within 30 minutes when the infants were born, and the supernatant was reserved after centrifuged. The levels of serum TLR-4, TNF-αand IL-6 were detected by enzyme-linked immunosorbent assay. Results The levels of TLR-4, TNF-αand IL-6 in idiopathic preterm and premature rupture of fetal membranes were signiifcantly higher than that in full-term group and showed positive correlation. Conclusion Cytokines TLR-4, TNF-αand IL-6 maybe closely related to the preterm birth.